High-resolution PTP1B inhibition profiling combined with high-performance liquid chromatography-high-resolution mass spectrometry-solid-phase extraction-nuclear magnetic resonance spectroscopy: Proof-of-concept and antidiabetic constituents in crude extract of Eremophila lucida

Fitoterapia
Yousof TahtahDan Staerk

Abstract

Type 2 diabetes (T2D) constituted 90% of the global 387 million diabetes cases in 2014. The enzyme protein-tyrosine phosphatase 1B (PTP1B) has been recognized as a therapeutic target for treatment of T2D and its adverse complications. With the aim of accelerating the investigation of complex natural sources, such as crude plant extracts, for potential PTP1B inhibitors, we have developed a bio-analytical platform combining high-resolution PTP1B inhibition profiling and high-performance liquid chromatography-high-resolution mass spectrometry-solid-phase extraction-nuclear magnetic resonance spectroscopy, i.e., HR-bioassay/HPLC-HRMS-SPE-NMR. Human recombinant PTP1B enzyme was used for the microplate-based PTP1B inhibition assay, which was optimized for pH and substrate concentration to be compatible with rate measurements within the 10min incubation time. Subsequently, analytical-scale HPLC-based microfractionation followed by colorimetric microplate-based PTP1B bioassaying enabled construction of a high-resolution inhibition profile corresponding to the HPLC profile. The high-resolution PTP1B inhibition profiling was validated using an artificial mixture of known PTP1B inhibitors and non-inhibiting compounds as negative controls....Continue Reading

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Citations

Jul 21, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Binh Thi Dieu TrinhDan Staerk
Feb 15, 2018·Computational and Mathematical Methods in Medicine·Xiangyu ZhangMaosheng Cheng
Dec 8, 2017·Archives of Pharmacal Research·Bing Tian ZhaoMi Hee Woo
Jan 30, 2021·Nature Reviews. Drug Discovery·Atanas G AtanasovClaudiu T Supuran
Jun 11, 2019·Journal of Agricultural and Food Chemistry·Chen-Chen ZhangJi-Jun Chen
Jul 30, 2021·The Plant Journal : for Cell and Molecular Biology·Oliver GerickeBirger Lindberg Møller

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